公开(公告)号：US08853204B2

公开(公告)日：2014-10-07

申请号：US10593666

申请日：2005-03-18

申请人： Kenneth Powell ,  Richard Kelsey ,  Malcolm Carter ,  Dagmar Alber ,  Lara Wilson ,  Elisa Henderson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms ,  Verity Dowdell

发明人： Kenneth Powell ,  Richard Kelsey ,  Malcolm Carter ,  Dagmar Alber ,  Lara Wilson ,  Elisa Henderson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms ,  Verity Dowdell

IPC分类号： A01N43/62 ,  A61K31/55 ,  A01N43/52 ,  A61K31/415 ,  C07D243/24 ,  C07D235/04 ,  A61K45/06 ,  A61K31/5513

CPC分类号： A61K45/06 ,  A61K31/5513 ,  A61K2300/00

摘要： A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.

摘要翻译： 一种药物组合物，其包含药学上可接受的载体或稀释剂，和：（a）RSV融合蛋白的抑制剂; 发现能够抑制RSV复制的苯并二氮杂衍生物对RSV具有高度活性。

公开(公告)号：US20070142403A1

公开(公告)日：2007-06-21

申请号：US10593666

申请日：2005-03-18

申请人： Kenneth Powell ,  Richard Kelsey ,  Malcolm Carter ,  Dagmar Alber ,  Lara Wilson ,  Elisa Henderson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms ,  Verity Dowdell

发明人： Kenneth Powell ,  Richard Kelsey ,  Malcolm Carter ,  Dagmar Alber ,  Lara Wilson ,  Elisa Henderson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms ,  Verity Dowdell

IPC分类号： A01N43/90

CPC分类号： A61K45/06 ,  A61K31/5513 ,  A61K2300/00

摘要： A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.

公开(公告)号：US20060040923A1

公开(公告)日：2006-02-23

申请号：US10528250

申请日：2003-09-22

申请人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

发明人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

IPC分类号： A61K31/5513 ,  C07D243/12

CPC分类号： C07D401/12 ,  C07D243/24 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV. Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; —each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, —CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; —n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(O)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6 hydroxyalkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

公开(公告)号：US08119630B2

公开(公告)日：2012-02-21

申请号：US12476797

申请日：2009-06-02

申请人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

发明人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

IPC分类号： A61P31/12

CPC分类号： C07D401/12 ,  C07D243/24 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; -each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; -n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(0)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6 hydroxyalkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

公开(公告)号：US20100015063A1

公开(公告)日：2010-01-21

申请号：US12476797

申请日：2009-06-02

申请人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

发明人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

IPC分类号： A61K9/12 ,  A61K38/20 ,  A61K31/56 ,  A61K31/5513 ,  C07D243/24

CPC分类号： C07D401/12 ,  C07D243/24 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; -each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; -n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(0)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6 hydroxyalkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

公开(公告)号：US07582624B2

公开(公告)日：2009-09-01

申请号：US10528250

申请日：2003-09-22

申请人： Malcolm Carter ,  Philip Chambers ,  Verity Dowdell ,  Elisa Ann Henderson ,  Richard David Kelsey ,  Debra Taylor ,  Stanley Tyms ,  Lara Wilson

发明人： Malcolm Carter ,  Philip Chambers ,  Verity Dowdell ,  Elisa Ann Henderson ,  Richard David Kelsey ,  Debra Taylor ,  Stanley Tyms ,  Lara Wilson

IPC分类号： C07D243/24 ,  C07D409/12 ,  C07D405/12 ,  C07D403/12 ,  A61K31/5513

CPC分类号： C07D401/12 ,  C07D243/24 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV. Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; —each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, —CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; —n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(O)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6 hydroxyalkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.